盐酸雷洛昔芬的合成研究

Synthesis of raloxifene hydrochloride

目的 盐酸雷洛昔芬的合成。方法 以 3 甲氧基苯硫酚为起始原料经过环合、脱甲氧基等反应 ,然后与 4 [2 (1 哌啶基 )乙氧基 ]苯甲酰氯发生Friedel Crafts反应 ,最后在巯基乙醇作用下脱去甲基保护得到盐酸雷洛昔芬。结果 合成产物经熔点、元素分析、经红外光谱、核磁共振谱等分析确定 ,结构正确 ;与文献报道一致。结论 与其它方法比较 ,该合成工艺简便 ,原料易得 。

OBJECTIVE To Synthesize Raloxifene Hydrochloride. METHOD Raloxifene was synthesized by cyclizing and demethoxylating of 3 methoxybenzenethiol, then treated with 4 [2 (1 pyrroldinyl)ethoxy]benzoyl chloride in the presence of monothioglycol to give Raloxifene Hydrochloride. RESULTS The melting point and element analsis, IR, 1HNMR of the product prepared were identical with that of the reported one.CONCLUSION The process can be easily controled and is suitable for a scale production.